Folwarczna J, Janiec W, Sliwiński L, Paruszewski R
Department of Pharmacology, Silesian School of Medicine, Sosnowiec, Poland.
Pol J Pharmacol Pharm. 1989 Nov-Dec;41(6):585-9.
The influence of nine new angiotensin II analogs: Asp-Arg-Val-Tyr-Gly-His-Pro-Phe (1-RP), Asp-Arg-Val-DL-p-ClPhe-Ile-His-Pro-Phe (2-RP), epsilon Ahx-Arg-Val-Tyr-Ile-His-Pro-Phe (3-RP), Asp-Arg-Val-Tyr-beta Ala-His-Pro-Ile (4-RP), Asp-Arg-Val-Tyr-Ile-Pro-Phe (5-RP), beta Ala-Arg-Val-Tyr-D-Val-His-Pro-Lac (6-RP), beta Ala-Arg-Val-Tyr-Ile-His-Pro-Lac (7-RP), epsilon Ahx-Val-Tyr-Ile-His-Pro-Phe (8-RP) and Arg-Val-Tyr-Ile-His-Pro-Thr (9-RP) on the contractility of small arterioles in the rat intestinal mesentery was investigated. All the peptides had weaker contractile activity than angiotensinamide. The most potent new peptides presented 56% (1-RP), 67% (3-RP) and 78% (8-RP) of the agonistic activity of angiotensinamide. None of the new angiotensin II analogs had antagonistic activity. Compounds 1-RP and 3-RP presented the tendency to cause tachyphylaxis.
研究了九种新型血管紧张素II类似物:天冬氨酸-精氨酸-缬氨酸-酪氨酸-甘氨酸-组氨酸-脯氨酸-苯丙氨酸(1-RP)、天冬氨酸-精氨酸-缬氨酸-DL-对氯苯丙氨酸-异亮氨酸-组氨酸-脯氨酸-苯丙氨酸(2-RP)、ε-氨基己酸-精氨酸-缬氨酸-酪氨酸-异亮氨酸-组氨酸-脯氨酸-苯丙氨酸(3-RP)、天冬氨酸-精氨酸-缬氨酸-酪氨酸-β-丙氨酸-组氨酸-脯氨酸-异亮氨酸(4-RP)、天冬氨酸-精氨酸-缬氨酸-酪氨酸-异亮氨酸-脯氨酸-苯丙氨酸(5-RP)、β-丙氨酸-精氨酸-缬氨酸-酪氨酸-D-缬氨酸-组氨酸-脯氨酸-乳糖(6-RP)、β-丙氨酸-精氨酸-缬氨酸-酪氨酸-异亮氨酸-组氨酸-脯氨酸-乳糖(7-RP)、ε-氨基己酸-缬氨酸-酪氨酸-异亮氨酸-组氨酸-脯氨酸-苯丙氨酸(8-RP)和精氨酸-缬氨酸-酪氨酸-异亮氨酸-组氨酸-脯氨酸-苏氨酸(9-RP)对大鼠肠系膜小动脉收缩性的影响。所有这些肽的收缩活性均弱于血管紧张素酰胺。最有效的新型肽呈现出血管紧张素酰胺激动活性的56%(1-RP)、67%(3-RP)和78%(8-RP)。新型血管紧张素II类似物均无拮抗活性。化合物1-RP和3-RP呈现出产生快速耐受性的趋势。